Global Patent Index - EP 1242361 A1

EP 1242361 A1 2002-09-25 - PROCESS OF PREPARING TOLTERODINE AND ANALOGUES THERE OF AS WELL AS INTERMEDIATES PREPARED IN THE PROCESS

Title (en)

PROCESS OF PREPARING TOLTERODINE AND ANALOGUES THERE OF AS WELL AS INTERMEDIATES PREPARED IN THE PROCESS

Title (de)

VERFAHREN FÜR DIE HERSTELLUNG VON TOLTERODINE UND DEREN ANALOGA SOWIE IM VERFAHREN HERGESTELLTE ZWISCHENPRODUKTE

Title (fr)

PROCEDE PERMETTANT DE PREPARER DE LA TOLTERODINE ET SES ANALOGUES, ET PRODUITS INTERMEDIAIRES PREPARES DANS CE PROCEDE

Publication

EP 1242361 A1 (EN)

Application

EP 00990151 A

Priority

  • SE 0002662 W
  • SE 9904850 A

Abstract (en)

[origin: WO0149649A1] The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprising the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II), wherein R>1<, R>2<, and R>3< independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb); b) subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb); c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form a corresponding enantiomerically enriched compound of formula (Va) or (Vb); d) converting the compound of formula (Va) or (Vb) to form the corresponding enantiomerically enriched compound of tolterodine or analogue thereof; and e) optionally converting a compound obtained in base form to a salt thereof, or converting a salt form to the free base. Formulas (IIIa), (IIIb), (IVa), (IVb), (Va) and (Vb) are specified in the application. The invention also relates to novel starting materials and intermediates used in the process.

IPC 1-7 (main, further and additional classification)

C07C 213/02; C07C 35/32; C07C 49/223; C07C 49/67; C07C 49/683; C07C 215/54; C07C 217/62; C07D 311/20

IPC 8 full level (invention and additional information)

C07D 311/14 (2006.01); C07B 53/00 (2006.01); C07B 61/00 (2006.01); C07C 29/143 (2006.01); C07C 35/32 (2006.01); C07C 45/51 (2006.01); C07C 45/65 (2006.01); C07C 45/66 (2006.01); C07C 45/74 (2006.01); C07C 49/223 (2006.01); C07C 49/67 (2006.01); C07C 49/683 (2006.01); C07C 49/807 (2006.01); C07C 49/835 (2006.01); C07C 213/00 (2006.01); C07C 213/02 (2006.01); C07C 215/54 (2006.01); C07C 217/62 (2006.01); C07D 311/20 (2006.01)

CPC (invention and additional information)

C07D 311/20 (2013.01); C07C 29/143 (2013.01); C07C 35/32 (2013.01); C07C 45/512 (2013.01); C07C 45/65 (2013.01); C07C 45/74 (2013.01); C07C 49/835 (2013.01); C07C 213/00 (2013.01); C07C 213/02 (2013.01); C07C 215/54 (2013.01); C07B 2200/07 (2013.01); C07C 2602/08 (2017.05)

Combination set (CPC)

  1. C07C 29/143 + C07C 35/32
  2. C07C 45/512 + C07C 49/67
  3. C07C 45/65 + C07C 49/67
  4. C07C 45/74 + C07C 49/813
  5. C07C 213/00 + C07C 215/54
  6. C07C 213/02 + C07C 215/54

Citation (search report)

See references of WO 0149649A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

DOCDB simple family

WO 0149649 A1 20010712; AR 027138 A1 20030312; AT 282019 T 20041115; AU 2719001 A 20010716; AU 782796 B2 20050901; BR 0016785 A 20020924; CA 2392832 A1 20010712; CN 1209342 C 20050706; CN 1414944 A 20030430; CZ 20022255 A3 20021113; DE 60015799 D1 20041216; DE 60015799 T2 20051215; DK 1242361 T3 20050214; EE 200200325 A 20030815; EP 1242361 A1 20020925; EP 1242361 B1 20041110; EP 1496045 A2 20050112; EP 1496045 A3 20050330; ES 2228658 T3 20050416; HK 1052000 A1 20050930; HU 0203816 A2 20030328; HU 0203816 A3 20041228; IL 150275 D0 20021201; JP 2003519207 A 20030617; MX PA02006415 A 20021129; MY 118906 A 20050228; NO 20023189 A 20020704; NO 20023189 D0 20020701; NZ 519079 A 20040227; PE 11232001 A1 20011109; PL 355947 A1 20040531; PT 1242361 E 20050131; SE 9904850 D0 19991230; SK 9392002 A3 20030109; TW I225476 B 20041221; US 2001016669 A1 20010823; US 6310248 B2 20011030; ZA 200204066 B 20030730